EP3651754B1 - Propion- und/oder buttersäure zur verwendung zur prophylaktischen und/oder unterstützenden therapeutischen behandlung von morbus parkinson - Google Patents
Propion- und/oder buttersäure zur verwendung zur prophylaktischen und/oder unterstützenden therapeutischen behandlung von morbus parkinson Download PDFInfo
- Publication number
- EP3651754B1 EP3651754B1 EP18750103.6A EP18750103A EP3651754B1 EP 3651754 B1 EP3651754 B1 EP 3651754B1 EP 18750103 A EP18750103 A EP 18750103A EP 3651754 B1 EP3651754 B1 EP 3651754B1
- Authority
- EP
- European Patent Office
- Prior art keywords
- salts
- agent
- use according
- butyric acid
- esters
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
- A23L33/115—Fatty acids or derivatives thereof; Fats or oils
- A23L33/12—Fatty acids or derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
- A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K33/00—Medicinal preparations containing inorganic active ingredients
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K33/00—Medicinal preparations containing inorganic active ingredients
- A61K33/06—Aluminium, calcium or magnesium; Compounds thereof, e.g. clay
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2200/00—Function of food ingredients
- A23V2200/30—Foods, ingredients or supplements having a functional effect on health
- A23V2200/322—Foods, ingredients or supplements having a functional effect on health having an effect on the health of the nervous system or on mental function
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2250/00—Food ingredients
- A23V2250/02—Acid
- A23V2250/05—Propionic acid
Definitions
- the invention relates to an agent for the prophylactic and/or supportive therapeutic treatment of Parkinson's disease.
- Numerous diseases are associated with intestinal microbiome imbalance, meaning the intestinal microbiome is out of balance, either due to intestinal imbalance or the loss of components essential for maintaining bodily functions.
- Significant changes in the intestinal microbiome can be detected in these diseases, such as obesity, ulcerative colitis, multiple sclerosis (MS), Parkinson's disease, and presumably also psychoses, as well as in rheumatic diseases and psoriasis. This suggests that the microbiome and disease are intertwined, either through a common cause or through mutual influence.
- the gut microbiome can be influenced by the type of food consumed and is able to adapt to the requirements of the particular diet. This means that a gut flora that is unfavorable to a patient's immune status can be modified through dietary interventions to improve the patient's immune status.
- the invention is based on the finding that Parkinson’s disease causes a characteristic change in the microbiome compared to healthy control subjects.
- bacteria that produce short-chain fatty acids are scarce or absent in the microbiome. Accordingly, there is a deficiency of short-chain fatty acids, which occur as breakdown products in the intestine of a healthy control subject. Braak postulated that Parkinson's disease begins in the intestine. This is consistent with the finding that transferring the microbiome from mice with Parkinson's disease to healthy mice produces a picture comparable to Parkinson's disease.
- Alpha-synuclein a transport protein found in the brain and involved in Parkinson's disease, can be detected in the intestines in very early stages of the disease and serves as an indicator of the disease. This also suggests a connection between the disease and what's happening in the intestines.
- Parkinson's disease Surprisingly, propionic acid and butyric acid have been shown to have a positive effect on the development and progression of Parkinson's disease. This also applies to their physiologically acceptable salts and esters. It has also been found that the targeted administration of these substances improves the drug treatment of Parkinson's disease, thus having a potentiating effect. In particular, the dosage of dopaminergic medications commonly used to treat Parkinson's disease can be significantly reduced.
- the invention relates to an agent for use in the prophylactic and/or supportive therapeutic treatment of Parkinson's disease, containing a physiologically effective amount of propionic acid and butyric acid and/or their physiologically acceptable salts or esters.
- the agent according to the invention can be administered for both prophylactic and therapeutic purposes to individuals predisposed to Parkinson's disease or to Parkinson's patients.
- the agent is particularly suitable for the supportive therapeutic treatment of Parkinson's patients who are otherwise undergoing conventional drug treatment.
- the agent according to the invention contains propionic acid and butyric acid, either alone or in combination.
- administration in the form of physiologically acceptable salts is preferred, with the emphasis on salts of physiologically important metals.
- physiologically important metals can include alkali and alkaline earth metal salts, as well as zinc and iron salts.
- propionic and butyric acid can also be administered in the form of their esters.
- the esters of C 1 to C 6 alcohols are used. in question, especially the methyl and ethyl esters.
- the esters are hydrolyzed in the body to form free acids.
- the agent according to the invention can be administered in conventional forms, for example, in the form of tablets, coated tablets, pills, capsules, lozenges, powders, and granules. Administration in liquid form is also possible, such as juices, drops, and teas. In any case, the agent is intended for oral administration.
- Preferred forms of administration are tablets, capsules, and powder.
- the tablets and capsules containing a unit dose of the agent according to the invention are preferably administered twice daily.
- the powder can, for example, be stirred into a drink or mixed with food.
- a unit dose for the above-mentioned dosage forms is in the range of 0.2 to 5 g, in particular 0.3 to 3 g.
- a particularly preferred amount for tablets, capsules, and powders is 0.5 to 2.0 g, each intended for morning and evening administration, and optionally also at midday, particularly in conjunction with meals.
- the weight ratio can, for example, be in the range of 3:1 to 1:3, in particular 3:2 to 2:3, for the total doses specified above.
- the agent according to the invention can be used for the supportive therapeutic treatment of Parkinson's patients.
- it is administered in addition to the usual drug treatment, for example, together with levodopa and other dopaminergic medications as commonly used.
- the dosage of the agent according to the invention is as stated above.
- butyric acid/butyrate The effects of butyric acid/butyrate have been investigated in patient studies involving more than 1,000 subjects, each lasting at least one year. A total of 6 g of butyric acid or butyrate (as salt) was administered together with the doctor's prescribed medication (levodopa, etc.) in three daily doses, morning, noon, and evening, with meals. Significant improvements in general health, particularly in motor function, were observed.
- Parkinson's patients treated with butyric acid/butyrate was reduced by at least 50%, and in some cases by up to 90%. This is particularly significant because the medication commonly used for Parkinson's patients, not only levodopa, leads to sometimes serious side effects, such as dizziness, nausea, tachyarrhythmia, psychosis, dyskinesia, and circulatory problems.
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Psychology (AREA)
- Inorganic Chemistry (AREA)
- Nutrition Science (AREA)
- Mycology (AREA)
- Polymers & Plastics (AREA)
- Food Science & Technology (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
- Coloring Foods And Improving Nutritive Qualities (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE102017115819.7A DE102017115819A1 (de) | 2017-07-13 | 2017-07-13 | Mittel zur prophylaktischen und/oder unterstützenden therapeutischen Behandlung von Morbus Parkinson |
| PCT/EP2018/069089 WO2019012108A1 (de) | 2017-07-13 | 2018-07-13 | Propion- und/oder buttersäure zur verwendung zur prophylaktischen und/oder unterstützenden therapeutischen behandlung von morbus parkinson |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| EP3651754A1 EP3651754A1 (de) | 2020-05-20 |
| EP3651754C0 EP3651754C0 (de) | 2025-04-30 |
| EP3651754B1 true EP3651754B1 (de) | 2025-04-30 |
Family
ID=63108510
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EP18750103.6A Active EP3651754B1 (de) | 2017-07-13 | 2018-07-13 | Propion- und/oder buttersäure zur verwendung zur prophylaktischen und/oder unterstützenden therapeutischen behandlung von morbus parkinson |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US20200163914A1 (enExample) |
| EP (1) | EP3651754B1 (enExample) |
| JP (1) | JP7206223B2 (enExample) |
| KR (1) | KR20200027976A (enExample) |
| CN (1) | CN110996933A (enExample) |
| AU (2) | AU2018298862A1 (enExample) |
| BR (1) | BR112020000570A2 (enExample) |
| CA (1) | CA3067728A1 (enExample) |
| DE (1) | DE102017115819A1 (enExample) |
| WO (1) | WO2019012108A1 (enExample) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2021048440A1 (en) | 2019-09-13 | 2021-03-18 | Basf Se | Composition for the treatment of neurodegenerative diseases |
| CN111450238A (zh) * | 2020-03-31 | 2020-07-28 | 上海交通大学医学院附属瑞金医院 | 骨钙素或丙酸在制备抗帕金森病药物中的应用 |
| CN113332266A (zh) * | 2021-06-10 | 2021-09-03 | 徐州医科大学 | 含丁酸的治疗与预防神经退行性疾病的药物及丁酸的应用 |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20060105962A1 (en) * | 2004-11-14 | 2006-05-18 | Robinson Robert O A | Tonic to maintain intestinal flora |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE19503598A1 (de) * | 1995-02-03 | 1996-08-08 | Zuzana Dr Cully | Verfahren zur fermentativen Herstellung von Propionsäure oder Buttersäure bzw. deren Salze |
| NL1009990C2 (nl) * | 1998-09-02 | 2000-03-15 | Sibeco Chemicals | Voedingssupplement en werkwijze voor het vervaardigen van zulk voedingssupplement. |
| WO2012095461A1 (de) * | 2011-01-12 | 2012-07-19 | Albert Daxer | Getränk |
| EP3019181A4 (en) * | 2013-07-09 | 2016-09-21 | Puretech Ventures Llc | COMPOSITIONS WITH COMBINATIONS OF BIOACTIVE MOLECULARS DERIVED FROM MICROBOTS FOR TREATING DISEASES |
| CN105055457A (zh) * | 2015-08-06 | 2015-11-18 | 温州医科大学附属第二医院 | 一种防治阿尔茨海默病的药物及其制备方法和应用 |
| DE102016103242A1 (de) * | 2016-02-24 | 2017-08-24 | Flexopharm Brain Gmbh & Co. Kg | Mittel zur unterstützenden Immunmodulation |
| WO2017091072A1 (en) * | 2015-11-27 | 2017-06-01 | Birrbeheer B.V. | Butyrate salts for use in inflammatory diseases |
| US11065217B2 (en) * | 2017-01-27 | 2021-07-20 | Temple University—Of the Commonwealth System of Higher Education | Use of short chain fatty acids for the treatment and prevention of diseases and disorders |
-
2017
- 2017-07-13 DE DE102017115819.7A patent/DE102017115819A1/de not_active Withdrawn
-
2018
- 2018-07-13 KR KR1020207003431A patent/KR20200027976A/ko not_active Ceased
- 2018-07-13 BR BR112020000570-3A patent/BR112020000570A2/pt not_active Application Discontinuation
- 2018-07-13 AU AU2018298862A patent/AU2018298862A1/en not_active Abandoned
- 2018-07-13 WO PCT/EP2018/069089 patent/WO2019012108A1/de not_active Ceased
- 2018-07-13 CN CN201880042374.6A patent/CN110996933A/zh active Pending
- 2018-07-13 US US16/627,688 patent/US20200163914A1/en not_active Abandoned
- 2018-07-13 EP EP18750103.6A patent/EP3651754B1/de active Active
- 2018-07-13 JP JP2019571280A patent/JP7206223B2/ja active Active
- 2018-07-13 CA CA3067728A patent/CA3067728A1/en active Pending
-
2021
- 2021-11-26 AU AU2021273627A patent/AU2021273627B2/en active Active
-
2022
- 2022-06-20 US US17/807,797 patent/US20220313634A1/en not_active Abandoned
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20060105962A1 (en) * | 2004-11-14 | 2006-05-18 | Robinson Robert O A | Tonic to maintain intestinal flora |
Also Published As
| Publication number | Publication date |
|---|---|
| US20200163914A1 (en) | 2020-05-28 |
| EP3651754A1 (de) | 2020-05-20 |
| DE102017115819A1 (de) | 2019-01-17 |
| KR20200027976A (ko) | 2020-03-13 |
| AU2021273627A1 (en) | 2021-12-16 |
| CA3067728A1 (en) | 2019-01-17 |
| BR112020000570A2 (pt) | 2020-07-14 |
| JP2020526485A (ja) | 2020-08-31 |
| CN110996933A (zh) | 2020-04-10 |
| WO2019012108A1 (de) | 2019-01-17 |
| US20220313634A1 (en) | 2022-10-06 |
| EP3651754C0 (de) | 2025-04-30 |
| AU2021273627B2 (en) | 2024-01-25 |
| JP7206223B2 (ja) | 2023-01-17 |
| AU2018298862A1 (en) | 2020-01-23 |
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